期刊
CHEMBIOCHEM
卷 18, 期 7, 页码 654-665出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201600642
关键词
angiogenesis; cyclodepsipeptidomimetics; inhibitors; integrins; peptidomimetics
资金
- Ministerio de Economia y Competividad (MEC, Spain) [IPT-010000-2011-2014]
- UPV/EHU [UFI QOSYC 11/22]
- Gobierno Vasco/Eusko Jaurlaritza [IG-2011/0000489, IT-628-13]
The alpha(v)beta(3) integrin receptor plays an important role in tumor metastasis and tumor-induced angiogenesis. The inhibition of this receptor with diverse ligands, antibodies, or cyclic peptides is a promising research field for the treatment of a variety of tumors. The replacement of Phe-(Me)Val dipeptide by a beta-lactam ring in Cilengitide has led to new products that show higher inhibitory activity than the parent cyclopeptide. In particular, substitution of a peptide bond beta-lactam-NH-Asp linkage by a beta-lactam-O-Asp ester linkage increases the activity of the new cyclodepsipeptide. In the same way it has been found that open-chain compounds of the form Asp-beta-lactam-Arg can interact with the receptor and inhibit its activity moderately. The integrin inhibitory activity of the synthesized compounds has been established by using the CGH array, a method that appears to be a more reliable trial than the classical adhesion test.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据